129655-21-6

129655-21-6 structure

Name: Bizelesin
Chemical Name: 1,3-bis[2-[(8S)-8-(chloromethyl)-4-hydroxy-1-methyl-7,8-dihydro-3H-pyrrolo[3,2-e]indole-6-carbonyl]-1H-indol-5-yl]urea
CAS Number: 129655-21-6
Molecular Formula: C₄₃H₃₆Cl₂N₈O₅
Molecular Weight: 815.70300
Catalog: Signaling Pathways Cell Cycle/DNA Damage DNA Alkylator/Crosslinker
Create Date: 2018-07-30 16:19:19
Modify Date: 2024-01-09 15:35:38
Bizelesin (NSC 615291; U-77779) is an AT-specific DNA alkylating agent that can generate DNA interstrand crosslinks, effectively inhibit DNA replication, and has potential anticancer activity[1].

Name	1,3-bis[2-[(8S)-8-(chloromethyl)-4-hydroxy-1-methyl-7,8-dihydro-3H-pyrrolo[3,2-e]indole-6-carbonyl]-1H-indol-5-yl]urea
Synonyms	Benzo(1,2-b:4,3-b')dipyrrol-4-ol,6,6'-(carbonylbis(imino-1H-indole-5,2-diylcarbonyl))bis(8-(chloromethyl)-3,6,7,8-tetrahydro-1-methyl-,(S-(R,R)) U-77,779 BIZELESIN Bizelesin (USAN/INN)

Description	Bizelesin (NSC 615291; U-77779) is an AT-specific DNA alkylating agent that can generate DNA interstrand crosslinks, effectively inhibit DNA replication, and has potential anticancer activity[1].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Cell Cycle/DNA Damage >> DNA Alkylator/Crosslinker
In Vitro	Bizelesin (0-5 μM, 4 h)可以通过靶向人类癌细胞 CEM 细胞中富含 AT的 DNA 域，造成 DNA 特异性损伤，进而造成癌细胞损伤，具有潜在的癌症治疗潜力[1]。 Bizelesin (0-500 nM)在 BSC-1 细胞中，当浓度为 10 nM 时导致 50% 的 DNA 合成抑制，相比之下，浓度为 160 nM 时才抑制 50% RNA 合成，而浓度高达至 200 nM 时也没有观察到蛋白质合成的抑制[2]。
References	[1]. J M Woynarowski, et al. AT-rich islands in genomic DNA as a novel target for AT-specific DNA-reactive antitumor drugs. J Biol Chem. 2001 Nov 2;276(44):40555-66. [2]. J M Woynarowski, et al. Effects of bizelesin (U-77,779), a bifunctional alkylating minor groove binder, on replication of genomic and simian virus 40 DNA in BSC-1 cells. Biochim Biophys Acta. 1997 Jul 17;1353(1):50-60.